RSC Advances最新文献

{"title":"Preparation and pharmacokinetic evaluation of a sertraline-methylpropyphenazone prodrug: a comparative metabolic study on the plasma and brain tissues of rats using LC-MS/MS analysis.","authors":"Alaa Khedr, Alanoud Ali, Tarek S Ibrahim, Ahmed K Kammoun","doi":"10.1039/d4ra08357a","DOIUrl":"10.1039/d4ra08357a","url":null,"abstract":"<p><p>A mutual prodrug of sertraline-methylpropyphenazone (SER-MP) was prepared and characterized using a spectral method. The yield of the prepared SER-MP was 90%, and its purity reached 98.8%. The metabolic fate of the prepared SER-MP <i>versus</i> sertraline (SER) was investigated in the plasma and brain tissues of rats. A solid-phase extraction procedure was developed and validated for the optimal recovery of SER, 3-hydroxymethylpropyphenazone (3-OHMP), and SER-MP from plasma and brain tissues. The extraction efficiency for the targeted analytes was improved from 93.5% to 98.0% using Chromabond® C8-100 mg solid-phase extraction columns. A high-performance liquid chromatography-triple-quad-mass spectrometric method was developed and validated to quantify the SER, SER-MP, and potential metabolites. The pharmacokinetic parameters showed that the time to reach the maximum plasma concentration (<i>t</i> _max) for both SER and SER-MP was 6 hours, and the maximum plasma concentration of SER-MP reached 192 ng mL^-1 with an elimination half-life time of 50 hours. The plasma level of SER, which was released as a metabolite of orally administered SER-MP, was increased by 2.4 times compared to SER HCl administered at equimolar doses. The concentration of SER-MP in the rat brains remained approximately stable at 100 ng g^-1 for 0.5 to 192 hours. The serotonin level in the rat brain homogenate was 50 to 90 ng g^-1 for both the group receiving SER and that receiving an equal molar dose of SER-MP. This observation was consistent during a time range of 1 to 192 h from oral administration. Thus, this approach could lead to the development of more efficient antidepressant therapies with reduced side effects. The findings indicate that SER-MP could minimize serotonin syndrome risks by maintaining steady serotonin levels in the brain, thus improving patient safety and compliance.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2800-2809"},"PeriodicalIF":3.9,"publicationDate":"2025-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11773334/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143057414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis, cytotoxicity, apoptosis-inducing activity and molecular docking studies of novel isatin-podophyllotoxin hybrids.","authors":"Ha Thanh Nguyen, Ket Tran Van, Hai Pham-The, Quang-Bao Le, Giang Le-Nhat-Thuy, Tuyet Anh Dang Thi, Phuong Hoang Thi, Quynh Giang Nguyen Thi, Anh Nguyen Tuan, Doan Vu Ngoc, Tuyen Van Nguyen","doi":"10.1039/d4ra08691k","DOIUrl":"10.1039/d4ra08691k","url":null,"abstract":"<p><p>Podophyllotoxin, along with its numerous derivatives and related compounds, is well known for its broad-spectrum pharmacological activity, especially for anticancer potential. In this study, several isatin-podophyllotoxin hybrid compounds were successfully synthesized with good yields through microwave-prompted three-component reactions of 2-amino-1,4-naphthoquinone, various substituted isatins, and tetronic acid. Their cytotoxicity was assessed against four types of human cancer cell lines, HepG2 (hepatoma carcinoma), MCF7 (breast cancer), A549 (non-small lung cancer), and KB (epidermoid carcinoma), alongside nontumorigenic HEK-293 human embryonic kidney cells. Among 14 compounds screened, 7f possessed the strongest cytotoxicity to KB and A549 cell lines, with IC₅₀ values of 1.99 ± 0.22 and 0.90 ± 0.09 μM, respectively. Further studies revealed that product 7f could arrest the cell cycle of A549 cells at S phase and induce apoptosis of A549 cells. This compound was examined for its binding ability against cyclin-dependent kinases (CDKs) and procaspase/caspase systems. The results indicated that 7f exhibited significant interactions with the residues of the ATP binding sites of CDK2/cyclin A and CDK5/p25 and also activated procaspase 6 through stable zinc chelation. Additionally, physicochemical and pharmacokinetic properties related to drug-likeness, in parallel with toxicity, were computationally assessed to identify the main issues that need to be addressed in structural optimization. Taken together, compound 7f was identified as a potent cytotoxic agent that could be considered for anticancer drug discovery and development.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2825-2839"},"PeriodicalIF":3.9,"publicationDate":"2025-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11774189/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143057428","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, synthesis, anti-inflammatory evaluation, and molecular docking studies of novel quinazoline-4(3<i>H</i>)-one-2-carbothioamide derivatives.","authors":"Le Thanh Hang Nguyen, Dinh Hoang Vu, Minh Quan Pham, Quoc Anh Ngo, Ngoc Binh Vo","doi":"10.1039/d4ra09094b","DOIUrl":"10.1039/d4ra09094b","url":null,"abstract":"<p><p>In this paper, a series of novel quinazoline-4(3<i>H</i>)-one-2-carbothioamide derivatives (8a-p) were designed and synthesized <i>via</i> the Wilgerodt-Kindler reaction between 2-methylquinazoline-4-one 10 and amines using S₈/DMSO as the oxidizing system. Their characteristics were confirmed by IR, NMR, HRMS spectra, and their melting point. These novel derivatives (8a-p) were evaluated for their anti-inflammatory activity by inhibiting NO production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophage cells. Compounds 8d (IC₅₀ = 2.99 μM), 8g (IC₅₀ = 3.27 μM), and 8k (IC₅₀ = 1.12 μM) exhibited potent inhibition of NO production compared to the standard drug dexamethasone (IC₅₀ = 14.20 μM). Compound 8a (IC₅₀ = 13.44 μM) exhibited NO inhibition comparable to dexamethasone. Structure-activity relationship (SAR) studies indicated that the presence of both the thioamide functional group (NH-C[double bond, length as m-dash]S) directly attached to the phenyl ring containing halogen substituents (4-Cl, 8d), (4-Br, 8g) and (4-CF₃, 8k), is responsible for the potent anti-inflammatory activity of these novel quinazolinone derivatives. Computational modeling studies revealed that compounds 8d, 8g, and 8k are potent inhibitors of TLR4 signaling through the formation of hydrophobic interactions and are stabilized by hydrogen bonds. Replacing the thioamide (8k) with an amide (8q) resulted in an 83-fold decrease in NO inhibitory potency. This highlights the important role of H-bonding involving the thioamide group. The structural shape difference results in favorable interactions of quinazolinones containing thioamide linkers compared to amide linkers to the target receptor. Furthermore, the ADMET profiles and physicochemical properties of these three lead compounds were predicted to meet the criteria for drug-like properties. Therefore, these compounds may be potential candidates for the treatment of many inflammatory diseases associated with immune disorders.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2850-2861"},"PeriodicalIF":3.9,"publicationDate":"2025-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11774271/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143057411","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Amino acid assisted synthesis of CDs: a novel paradigm in plant tissue culture media for enhanced cellular effects and biotechnological advancements.","authors":"C Annmary, Bitty Joseph, N J Simi, V V Ison","doi":"10.1039/d4ra08776c","DOIUrl":"10.1039/d4ra08776c","url":null,"abstract":"<p><p>We report a green approach to prepare carbon dots (CDs) with fresh tomatoes as carbon sources and amino acids as dopants (ACDs) by a microwave assisted method. The synthesised CDs were analysed by UV-visible absorption spectroscopy, photoluminescence spectroscopy, high resolution transmission electron spectroscopy, X-ray diffraction, Fourier transform infrared spectroscopy, X-ray photo electron spectroscopy. An MTT assay was used to evaluate the cytotoxicity of CDs toward L929 cells and found that CDs exhibit low cytotoxicity. The effects of ACDs on seed germination were evaluated by treating pea seeds with various concentrations of CDs. The results demonstrated a significant increase in germination and seedling vigour compared to untreated controls. Subsequently, the application of ACDs was extended to plant tissue culture. Explants treated with ACDs exhibited enhanced growth and development, indicating improved morphogenesis and proliferation rates. This study highlights the potential of ACDs as an efficient, non-toxic growth promoter in both seed germination and plant tissue culture, paving the way for their application in sustainable agriculture and plant biotechnology.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2759-2765"},"PeriodicalIF":3.9,"publicationDate":"2025-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11774188/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143057542","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A cost-effective and innovative detector for iron ions.","authors":"Yanhui Guo, Jiayi Zhu, Yumei Dai, Long Chen, Weibing Li, Zihang Yuan, Jie Zhou, En Tang","doi":"10.1039/d4ra08065c","DOIUrl":"10.1039/d4ra08065c","url":null,"abstract":"<p><p>Severe environmental contamination can result from high concentrations of iron ions, which can have a detrimental impact on human health and well-being. Consequently, it is imperative to develop novel materials that can address environmental issues. Metal-organic frameworks (MOFs) possess unique properties that render them efficient fluorescent probes for the rapid and precise detection of these pollutants. A diverse array of MOF probes have been developed to detect iron ions. Nevertheless, their practical application is significantly impeded by the high production cost, which is a critical factor. This raises the question: why not implement a cost-effective, sensitive detector instead? Our research group has developed a novel MOF material, [Zn₂(bpy)(APA)₂(H₂O)] _<i>n</i> , that is specifically designed for MOF-based \"off\" sensors in aqueous media. This material not only demonstrates high sensitivity, and is manufactured from low-cost raw materials, but it also holds significant commercial potential, with production costs that are 98.4% lower than those of existing alternatives.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2645-2650"},"PeriodicalIF":3.9,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11770415/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143050964","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Hard template-salt template double template preparation of heteroatom-doped hierarchical porous carbon and its electrochemical properties.","authors":"Fangfang Liu, Fenglei Zhang, Jinan Niu","doi":"10.1039/d4ra08818b","DOIUrl":"10.1039/d4ra08818b","url":null,"abstract":"<p><p>Heteroatom-doped hierarchical porous carbon (AF-MMTC) was prepared with hard template and salt template dual templating agents, and the effects of salt template additions on its micro-morphology, pore structure, specific surface area and electrochemical properties were investigated. The salt template not only acts as a template, but also plays the role of a pore-making agent. AF-MMTC5 has a high specific surface area of 1772 m² g^-1, a 41% microporous content and 1.8 at% nitrogen content. The electrochemical test results show that the specific capacitance of AF-MMTC5 is 231.9 F g^-1 (0.5 A g^-1) in the three-electrode system, and the capacity retention can reach 98.5% after 5000 cycles; in the two-electrode system, the specific capacitance of AF-MMTC5 can reach 216.3 F g^-1 when the current density is 0.5 A g^-1, and the specific capacitance can still reach 172.2 F g^-1 when the current density is increased to 20 A g^-1. AF-MMTC5 represents the highest energy density of 4.81 W h kg^-1 at the power density of 50 W kg^-1. And the capacity retention rates of AF-MMTC5 is 85.1%. The good electrochemical properties of AF-MMTC5 indicate that it has great potential for application in supercapacitor electrode materials. In addition, the results provide useful information for the preparation of hierarchical porous carbon with high specific surface area.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2582-2590"},"PeriodicalIF":3.9,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11770366/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143050996","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Correction: Design, synthesis, and <i>in silico</i> studies of new quinazolinones tagged thiophene, thienopyrimidine, and thienopyridine scaffolds as antiproliferative agents with potential p38α MAPK kinase inhibitory effects.","authors":"Aisha A Alsfouk, Ismail M M Othman, Manal M Anwar, Asmaa Saleh, Eman S Nossier","doi":"10.1039/d5ra90011e","DOIUrl":"https://doi.org/10.1039/d5ra90011e","url":null,"abstract":"<p><p>[This corrects the article DOI: 10.1039/D4RA06744D.].</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2758"},"PeriodicalIF":3.9,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11770409/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143050986","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>Moringa oleifera</i> leaves extract-mediated synthesis of ZnO nanostructures for the enhanced photocatalytic oxidation of erythrosine.","authors":"Noshaba Parven, Khalida Faryal Almani, Muhammad Ali Bhatti, Aneela Tahira, Omm-E-Hany, Aqeel Ahmed Shah, Ayman Nafady, Matteo Tonezzer, Zafar Hussain Ibupoto","doi":"10.1039/d4ra08782h","DOIUrl":"10.1039/d4ra08782h","url":null,"abstract":"<p><p>This study was focused on the development of ZnO nanostructures for the efficient oxidation of erythrosine dye and for studying the antibacterial activity of ZnO. It was observed that the phytochemicals from <i>Moringa oleifera</i> leaves modified the size, shape, crystalline properties and surface chemical composition of the ZnO nanostructures. ZnO nanostructures synthesized with 15 mL <i>Moringa oleifera</i> leaves extract (S-15) demonstrated highly efficient oxidation of erythrosine dye under the illumination of natural sunlight. Various photocatalyst evaluation parameters, such as initial dye concentration, pH of the dye solution, catalyst dose and cycling stability, were studied. The S-15 sample of ZnO exhibited almost 100% dye removal in an alkaline pH of 12 and a low concentration of 4.54 × 10^-5 M. Furthermore, improved antibacterial activity was also observed against <i>E. coli</i> and <i>Bacillus subtilis</i> bacteria strains. The use of <i>Moringa oleifera</i> leaves extract could be considered a low-cost, facile and ecofriendly green synthesis protocol for replacing the use of toxic chemicals and for eliminating the risk of releasing of toxic chemicals into the environment during the synthesis of high-performance nanostructured materials.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2810-2824"},"PeriodicalIF":3.9,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11771134/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143050959","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Facile preparation of multifunctional biomaterials BTO/Ag and their applications in photoelectrochemical sensing, photodegradation and antibacterial activities.","authors":"Zhang Kexi, Yan Bingdong, Chen Delun, Wang Xiaohong, Cao Yang, Zhang Xuewei, Hao Wanjun, Tu Jinchun","doi":"10.1039/d4ra07385a","DOIUrl":"10.1039/d4ra07385a","url":null,"abstract":"<p><p>With the progress of modern technology and the diversification of societal demands, traditional materials with single properties can no longer meet the requirements of complex and constantly evolving application scenarios. To tackle intricate biomedical applications like disease diagnosis and treatment, scientists are focusing on exploring the design of novel multifunctional biomaterials that possess diverse activities. Bismuth titanate (Bi₄Ti₃O₁₂, BTO), which has multifunctionality and great application potential, unfortunately suffers from inadequate photocatalytic performance. On the other hand, silver nanoparticles (Ag), known for their antibacterial properties, have relatively limited functions. In this study, we overcame these limitations by combining BTO with Ag to form a BTO/Ag biomultifunctional material. Our experiments showed that the addition of Ag effectively improved BTO's UV absorption ability, decreased electron transfer resistance, and increased carrier concentration. As a result, the photocatalytic performance of BTO/Ag was significantly enhanced, and its photoelectrochemical sensing and photodegradation capabilities were also greatly improved. Moreover, BTO served as an effective substrate, preventing Ag from agglomerating and maximizing its antibacterial potential. In specific performance evaluations, ascorbic acid and methylene blue (MB) were used to study the photoelectrochemical sensing and photodegradation capabilities respectively, while <i>Escherichia coli</i> and <i>Staphylococcus aureus</i> were chosen as test organisms to assess the antibacterial properties. All in all, this research has yielded promising results.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2657-2667"},"PeriodicalIF":3.9,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11770675/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143050994","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"High energy density solid state symmetric supercapacitors using ionic liquid dispersed Li⁺ ion-perovskites.","authors":"Bhargab Sharma, Shrishti Sharma, Gurpreet Kaur, Hardeep, Anshuman Dalvi","doi":"10.1039/d4ra07417c","DOIUrl":"10.1039/d4ra07417c","url":null,"abstract":"<p><p>The study reports solid-state ceramic supercapacitors (SSCs) assembled using a novel composite electrolyte based on Li⁺ ion conducting perovskite-type LLTO (Li_0.34La_0.51TiO₃) and an ionic liquid (EMIM BF₄). Small amounts of various ionic liquids (ILs) were added to LLTO to enhance the ionic conductivity and improve electrode compatibility. The optimal composition with approximately ∼6 wt% EMIM BF₄ in LLTO exhibited a high ionic conductivity of around ∼10^-3 Ω^-1 cm^-1 at room temperature, nearly three orders of magnitude higher than that of the pristine LLTO. Optimized electrolyte composition was therefore used for fabrication by compressing between high surface area activated carbon-coated copper electrodes and assembled in an affordable lamination cell geometry. The SSCs demonstrated stable cycling performance for at least 10 000 cycles at 2 V operating voltage and 1.13 A g^-1 (2 mA) discharge current, with a remarkably high coulombic efficiency of ∼99%. A typical laminated cell at 35 °C exhibited a specific capacitance of around 510 F g^-1 at 0.57 A g^-1 (1 mA), and 2 V. Supercapacitors operating below 2 V showed a pure electric double-layer type nature. A stack of 4 cells in series can power two white LEDs (6 V) for ∼40 minutes.</p>","PeriodicalId":102,"journal":{"name":"RSC Advances","volume":"15 4","pages":"2704-2716"},"PeriodicalIF":3.9,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11770677/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143051011","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}